PREGNENOLONE MONOSULFATE

生物活性靶点体外研究体内研究 PREGNENOLONE MONOSULFATE 试剂级价格

CAS号:1247-64-9
英文名:(3S,8S,9R,10S,13S,14R,17R)-17-acetyl-10,13-dimethyl-3-sulfooxy-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthrene
中文名:PREGNENOLONE MONOSULFATE
CBNumber:CB01236206
分子式:C21H32O5S
分子量:396.54
MOL File:1247-64-9.mol

PREGNENOLONE MONOSULFATE化学性质

密度 :1.25±0.1 g/cm3(Predicted)
储存条件 :Store at -20°C,stored under nitrogen
溶解度 :DMSO: 62.5 mg/mL (157.61 mM)
酸度系数(pKa) :-3.51±0.18(Predicted)
形态 :Solid
颜色 :White to off-white

PREGNENOLONE MONOSULFATE性质、用途与生产工艺

生物活性 Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) 是一种功能强大的神经甾体，是包括甾体酮在内的各种甾体激素的主要前体。Pregnenolone monosulfate 是大麻素 CB1 受体的信号传导特异性抑制剂，抑制由 CB1 受体介导的四氢大麻酚 (THC) 的作用。Pregnenolone monosulfate 可以保护大脑免受大麻中毒。
靶点

CB1

Human Endogenous Metabolite
体外研究

CB1 receptor stimulation increases brain Pregnenolone levels, which in turn exerts a negative feedback on the activity of the CB1 receptor antagonizing most of the known behavioral and somatic effects of THC. Pregnenolone likely acts as a signaling-specific negative allosteric modulator binding to a site distinct from that occupied by orthosteric ligands. Pregnenolone does not modify agonist binding but only agonist efficacy.
The effect of THC is significantly attenuated when slices are pre-treated with Pregnenolone 100 nM (15.1±1.8 % of inhibition). These effects are likely due to a pre-synaptic action of Pregnenolone. Thus, Pregnenolone blocks the increase in paired-pulse ratio (PPR) induced by THC but does not modify either the amplitude or the decay time of miniature EPSC (mEPSC).
体内研究

Pregnenolone administration (2-6 mg/kg) blocks THC-induced food-intake in Wistar rats and in C57BL/6N mice, and blunts the memory impairment induced by THC in mice, but it does not modify these behaviors per se . Injections of Pregnenolone (2 and 4mg/kg) before each self-administration session reduce the intake of WIN 55,212-2 and reduce the break-point in a progressive ratio schedule.